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GS-6201

SKU: orb1308258

Description

GS-6201 (CVT-6883) is a potent and selective adenosine A2B receptor antagonist with a Ki of 22 nM for the human receptor. This small molecule is a valuable research tool for investigating the role of A2B signaling in areas such as fibrosis, inflammation, and cancer in both cellular and animal models.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Images & Validation

Key Properties

CAS Number752222-83-6
MW446.43
Purity99.94% (May vary between batches)
FormulaC21H21F3N6O2
SMILESCCCn1c(=O)n(CC)c2[nH]c(nc2c1=O)-c1cnn(Cc2cccc(c2)C(F)(F)F)c1
TargetAdenosine Receptor
Solubility10% DMSO+90% Corn Oil:2 mg/mL (4.48 mM);DMSO:30 mg/mL (67.2 mM)

Bioactivity

Target IC50
A2A:3280 nM(Ki, human)|A2B:22 nM(Ki, human)|A3:1070 nM(Ki, human)|A1:1940 nM(Ki, human)
In Vivo
GS-6201 (2 mg/kg; p.o.) treatment displays the Cmax, dAUC and t1/2 are 1110 ng/mL, 6500 ng h/mL, and 4.25 hours, respectively . GS-6201 (4 mg/kg; i.p.; every 12 h for 14 days) obviously decreases IL-6, TNF-α, E-selectin, ICAM-1, and VCAM plasma levels. GS-6201 (4 mg/kg; i.p.; every 12 h for 14 days) causes an obvious attenuation of left and right ventricular enlargement and dysfunction at 7 days, which was maintained at 14 days and also at 28 days .

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

human A1 receptors, human A2A receptors, human A2B receptors, human A3 receptors, GS6201, GS-6201, GS 6201, inhibit, Inhibitor, infarction, myocardial, caspase-1, cardiac, CVT 6883, CVT-6883, CVT6883, A2B, acute, airway, affinity, Adenosine Receptor, AdenosineReceptor, selectivity, P1 receptor, reactivity, remodeling
Quality Guarantee

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at support@biorbyt.com.

Key Properties

No computed properties available.

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Protocol Information

GS-6201 (orb1308258)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

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1 mg
$ 70.00
1 ml x 10 mM (in DMSO)
$ 120.00
5 mg
$ 120.00
10 mg
$ 170.00
25 mg
$ 320.00
50 mg
$ 490.00
100 mg
$ 710.00
200 mg
$ 980.00
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